Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.11.2 extracted from

  • Grembecka, J.; Mucha, A.; Cierpicki, T.; Kafarski, P.
    The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity (2003), J. Med. Chem., 46, 2641-2655.
    View publication on PubMed
Search for more literature for 3.4.11.2

Application

Application Comment Organism
medicine enzyme is a target for inhibitor design Sus scrofa

Inhibitors

Inhibitors Comment Organism Structure
2-[[(1-amino-3-methylbutyl)hydroxyphosphinyl]methyl]-4-methylpentanoic acid (R)-isomer and 1:1 ratio of the 2 diastereomers Sus scrofa
2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-3-(4-hydroxyphenyl)propionic acid
-
 Sus scrofa
2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-3-phenylpropionic acid
-
 Sus scrofa
2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-4-methylpentanoic acid
-
 Sus scrofa
3-[(1-amino-3-methylbutyl)hydroxyphosphinyl]-propionic acid
-
 Sus scrofa
additional information computational inhibitor design, inhibition mechanism, structural requirements of phosphinate inhibitors for binding and inhibition, overview Sus scrofa
N-[(1-hydroxy-3-methylbutyl)oxyphosphinyl]glycine dilithium salt
-
 Sus scrofa

Organism

Organism UniProt Comment Textmining
Sus scrofa
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
 Sus scrofa
-
kidney
-
 Sus scrofa
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-Leu-4-nitroanilide + H2O
-
 Sus scrofa L-Leu + 4-nitroaniline
-
 ?

Synonyms

Synonyms Comment Organism
aminopeptidase N
-
 Sus scrofa
APN
-
 Sus scrofa

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000036
-
 2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-3-(4-hydroxyphenyl)propionic acid pH 8.4, 25°C Sus scrofa
0.000276
-
 2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-3-phenylpropionic acid pH 8.4, 25°C Sus scrofa
0.001
-
 2-[[(1-amino-4-phenylbutyl)hydroxyphosphinyl]methyl]-4-methylpentanoic acid pH 8.4, 25°C Sus scrofa
0.00102
-
 2-[[(1-amino-3-methylbutyl)hydroxyphosphinyl]methyl]-4-methylpentanoic acid pH 8.4, 25°C, 1:1 ratio of the 2 diastereomers Sus scrofa
0.00142
-
 3-[(1-amino-3-methylbutyl)hydroxyphosphinyl]-propionic acid pH 8.4, 25°C Sus scrofa